SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC 50 =18, 15, and 38?nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.
性状
Solid
IC50 & Target[1][2]
hGlyT1 18 nM (IC50) rGlyT1 15 nM (IC5
体外研究(In Vitro)
SSR504734 (15 nM-86 μM; 10 min) inhibits glycine uptake in human SK-N-MC and rat C6 cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability AssayCell Line:
体内研究(In Vivo)
SSR504734 (i.p. and p.o.; 1-100 mg/kg; once) treatment shows good oral bioavailability.
SSR504734 (i.p.; 30 mg/kg; once) induces a rapid and significant decrease of specific glycine uptake.
SSR504734 (i.p.; 10 mg/kg; once) increases extracellular levels of Glycine in the prefrontal cortex (PFC) of freely moving rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Ronan Depoortère, et al. Neurochemical, electrophysiological and pharmacological profiles of the selective inhibitor of the glycine transporter-1 SSR504734, a potential new type of antipsychotic. Neuropsychopharmacology. 2005 Nov;30(11):1963-85.
溶解度数据
In Vitro: DMSO : 100 mg/mL (230.79 mM; Need ultrasonic)配制储备液